2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. BX-513

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with Ki values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis.

For research use only. We do not sell to patients.

BX-513

BX-513 Chemical Structure

CAS No. : 193542-65-3

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BX-513 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with Ki values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis[1].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.63 μM
Compound: 23
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells
[PMID: 12166951]
CHO IC50
9 μM
Compound: 23
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells
[PMID: 12166951]
COS-7 EC50
3.2 μM
Compound: 1 table-1
Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
[PMID: 16190772]
COS-7 IC50
9.3 μM
Compound: 1 table-1
Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL5
Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL5
[PMID: 16190772]
HEK293 EC50
4.5 μM
Compound: VUF2274
Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay
[PMID: 21784633]
HEK293 IC50
2.5 μM
Compound: 6s
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor
[PMID: 10579830]
HEK-293T EC50
>10 μM
Compound: VUF2274
Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay
Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay
[PMID: 25052428]
HEK-293T EC50
4.5 μM
Compound: VUF2274
Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay
[PMID: 25052428]
In Vitro

BX-513 (Compound 1) (30-1000 nM) dose-dependently inhibits MIP-1α-induced extracellular acidification in THP-1 cells, with an IC50 of 124 nM, and also suppresses RANTES-induced acidification in these cells[1].
BX-513 (100-1000 nM) inhibits CCR1-expressing HEK 293 cells in a dose-dependent manner, with an IC50 of approximately 200 nM. This compound has no intrinsic agonist activity, exerts reversible inhibitory effects, and also inhibits RANTES-induced intracellular Ca2+ mobilization in these cells[1].
BX-513 (20-2000 nM) dose-dependently inhibits MIP-1α- and RANTES-induced chemotaxis of human peripheral blood mononuclear cells (PBMCs), without affecting migration induced by other chemokines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BX-513 Related Antibodies
Clinical Trial
Molecular Weight

445.00

Formula

C28H29ClN2O
CAS No.
SMILES

N#CC(C=1C=CC=CC1)(C=2C=CC=CC2)CCCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BX-513 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BX-513193542-65-3VUF 2274BX513BX 513VUF2274VUF-2274CCRCC chemokine receptorrheumatoid arthritisG-protein-coupled receptorsTHP-1 cellsMIP-1αseven-transmembrane domain receptorsperipheral blood mononuclear cellCCR1 chemokine receptorHEK 293 cellsRANTESmultiple sclerosisInhibitorinhibitorinhibit

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